Cat. No. Name Size Price Add Cart
KI2440JNJ-264815851 mg$140
JNJ-264815855 mg$336
JNJ-2648158510 mg$592
JNJ-2648158550 mg$1636
JNJ-26481585100 mg$2840

Chemical Characteristic

Product NameJNJ-26481585
SynonymsN/A
CAS No.875320-29-9
Molecular Weight 394.47
FormulaC21H26N6O2
Chemical NameN-hydroxy-2-(4-(((1-methyl-1H-indol-3-yl)methylamino)methyl)piperidin-1-yl)pyrimidine-5-carboxamide
Smilesc1(ncc(cn1)C(=O)NO)N1CCC(CC1)CNCc1cn(c2c1cccc2)C
Chemical Structure

Biological activities

JNJ-26481585 is a novel pan histone deacetylase (HDAC) inhibitor. JNJ-26481585 has high potency towards class I HDAC enzymes (HDAC 1, 2 and 3) with IC50s of 0.11, 0.33 and 4.8 nM, respectively.[1] JNJ-26481585 also inhibits HDAC4, HDAC10 and HDAC11 with IC50s of 0.64, 0.46 and 0.37 nM, respectively. JNJ-26481585 inhibits the proliferation of hematologic tumor cell lines in all lung, breast, colon, prostate, brain, and ovarian tumor cell lines tested, with IC50s ranging from 3.1 to 246 nM. Oral administration of JNJ-26481585 induces continuous histone H3 acetylation in NMRI nu/nu mice.[2]

Protocols

In vitro, JNJ-26481585 is prepared in DMSO.[2]

References

[1] Deleu S, et al. The effects of JNJ-26481585, a novel hydroxamate-based histone deacetylase inhibitor, on the development of multiple myeloma in the 5T2MM and 5T33MM murine models. Leukemia. 2009, 23(10): 1894-1903.
[2] Arts J, et al. JNJ-26481585, a novel "second-generation" oral histone deacetylase inhibitor, shows broad-spectrum preclinical antitumoral activity. Clin Cancer Res. 2009, 15(22): 6841-6851.

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